All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

inclisiran 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
small interfering RNA including siRNA, miRNA and piRNA	5498	1639324-58-5

Description:

Molecule

Description

Molfile Synonyms: inclisiran leqvio ALN-PCSsc ALN-60212 KJX-839 PCSK9si

Inclisiran is a double-stranded small interfering ribonucleic acid (siRNA), conjugated on the sense strand with triantennary N-Acetylgalactosamine (GalNAc) to facilitate uptake by hepatocytes. In hepatocytes, inclisiran utilizes the RNA interference mechanism and directs catalytic breakdown of mRNA for PCSK9. This increases LDL-C receptor recycling and expression on the hepatocyte cell surface, which increases LDL-C uptake and lowers LDL-C levels in the circulation. Molecular weight: Formula: CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: ALOGS: ROTB: None

Drug dosage:

Dose	Unit	Route
1.60	mg	P

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Dec. 9, 2020	EMA	Novartis Europharm Limited
Dec. 22, 2021	FDA	NOVARTIS PHARMS CORP

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Low density lipoprotein increased	124.09	43.53	25	631	6332	63482034
Myalgia	93.63	43.53	40	616	146489	63341877

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Myalgia	99.94	41.02	38	411	84072	34872410
Low density lipoprotein increased	68.91	41.02	15	434	4421	34952061

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Myalgia	103.43	43.27	41	515	185600	79558232
Low density lipoprotein increased	62.54	43.27	14	542	8608	79735224

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C10AX16	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, PLAIN Other lipid modifying agents

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Atherosclerotic cardiovascular disease	indication	72092001
Familial hypercholesterolemia - heterozygous	indication	238079002

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 284MG BASE/1.5ML (EQ 189MG BASE/ML)	LEQVIO	NOVARTIS	N214012	Dec. 22, 2021	RX	SOLUTION	SUBCUTANEOUS	10266825	Nov. 4, 2023	AS AN ADJUNCT TO DIET AND STATIN THERAPY FOR THE TREATMENT OF ADULTS WITH PRIMARY HYPERLIPIDEMIA, INCLUDING HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA (HEFH), BY INHIBITING EXPRESSION OF THE PCSK9 GENE
EQ 284MG BASE/1.5ML (EQ 189MG BASE/ML)	LEQVIO	NOVARTIS	N214012	Dec. 22, 2021	RX	SOLUTION	SUBCUTANEOUS	11078485	Nov. 4, 2023	AS AN ADJUNCT TO DIET AND STATIN THERAPY FOR THE TREATMENT OF ADULTS WITH PRIMARY HYPERLIPIDEMIA, INCLUDING HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA (HEFH), BY INHIBITING EXPRESSION OF THE PCSK9 GENE
EQ 284MG BASE/1.5ML (EQ 189MG BASE/ML)	LEQVIO	NOVARTIS	N214012	Dec. 22, 2021	RX	SOLUTION	SUBCUTANEOUS	9708610	Jan. 1, 2024	AS AN ADJUNCT TO DIET AND STATIN THERAPY FOR THE TREATMENT OF ADULTS WITH PRIMARY HYPERLIPIDEMIA, INCLUDING HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA (HEFH), BY INHIBITING EXPRESSION OF THE PCSK9 GENE
EQ 284MG BASE/1.5ML (EQ 189MG BASE/ML)	LEQVIO	NOVARTIS	N214012	Dec. 22, 2021	RX	SOLUTION	SUBCUTANEOUS	8809292	May 10, 2027	AS AN ADJUNCT TO DIET AND STATIN THERAPY FOR THE TREATMENT OF ADULTS WITH PRIMARY HYPERLIPIDEMIA, INCLUDING HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA (HEFH), BY INHIBITING EXPRESSION OF THE PCSK9 GENE
EQ 284MG BASE/1.5ML (EQ 189MG BASE/ML)	LEQVIO	NOVARTIS	N214012	Dec. 22, 2021	RX	SOLUTION	SUBCUTANEOUS	8222222	Dec. 29, 2027	AS AN ADJUNCT TO DIET AND STATIN THERAPY FOR THE TREATMENT OF ADULTS WITH PRIMARY HYPERLIPIDEMIA, INCLUDING HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA (HEFH), BY INHIBITING EXPRESSION OF THE PCSK9 GENE
EQ 284MG BASE/1.5ML (EQ 189MG BASE/ML)	LEQVIO	NOVARTIS	N214012	Dec. 22, 2021	RX	SOLUTION	SUBCUTANEOUS	10131907	Aug. 24, 2028	AS AN ADJUNCT TO DIET AND STATIN THERAPY FOR THE TREATMENT OF ADULTS WITH PRIMARY HYPERLIPIDEMIA, INCLUDING HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA (HEFH), BY INHIBITING EXPRESSION OF THE PCSK9 GENE
EQ 284MG BASE/1.5ML (EQ 189MG BASE/ML)	LEQVIO	NOVARTIS	N214012	Dec. 22, 2021	RX	SOLUTION	SUBCUTANEOUS	8828956	Dec. 4, 2028	AS AN ADJUNCT TO DIET AND STATIN THERAPY FOR THE TREATMENT OF ADULTS WITH PRIMARY HYPERLIPIDEMIA, INCLUDING HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA (HEFH), BY INHIBITING EXPRESSION OF THE PCSK9 GENE
EQ 284MG BASE/1.5ML (EQ 189MG BASE/ML)	LEQVIO	NOVARTIS	N214012	Dec. 22, 2021	RX	SOLUTION	SUBCUTANEOUS	9370582	Dec. 4, 2028	AS AN ADJUNCT TO DIET AND STATIN THERAPY FOR THE TREATMENT OF ADULTS WITH PRIMARY HYPERLIPIDEMIA, INCLUDING HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA (HEFH), BY INHIBITING EXPRESSION OF THE PCSK9 GENE
EQ 284MG BASE/1.5ML (EQ 189MG BASE/ML)	LEQVIO	NOVARTIS	N214012	Dec. 22, 2021	RX	SOLUTION	SUBCUTANEOUS	8106022	Dec. 12, 2029	AS AN ADJUNCT TO DIET AND STATIN THERAPY FOR THE TREATMENT OF ADULTS WITH PRIMARY HYPERLIPIDEMIA, INCLUDING HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA (HEFH), BY INHIBITING EXPRESSION OF THE PCSK9 GENE
EQ 284MG BASE/1.5ML (EQ 189MG BASE/ML)	LEQVIO	NOVARTIS	N214012	Dec. 22, 2021	RX	SOLUTION	SUBCUTANEOUS	10125369	Aug. 18, 2034	AS AN ADJUNCT TO DIET AND STATIN THERAPY FOR THE TREATMENT OF ADULTS WITH PRIMARY HYPERLIPIDEMIA, INCLUDING HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA (HEFH), BY INHIBITING EXPRESSION OF THE PCSK9 GENE
EQ 284MG BASE/1.5ML (EQ 189MG BASE/ML)	LEQVIO	NOVARTIS	N214012	Dec. 22, 2021	RX	SOLUTION	SUBCUTANEOUS	10851377	Aug. 25, 2036	AS AN ADJUNCT TO DIET AND STATIN THERAPY FOR THE TREATMENT OF ADULTS WITH PRIMARY HYPERLIPIDEMIA, INCLUDING HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA (HEFH), BY INHIBITING EXPRESSION OF THE PCSK9 GENE

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 284MG BASE/1.5ML (EQ 189MG BASE/ML)	LEQVIO	NOVARTIS	N214012	Dec. 22, 2021	RX	SOLUTION	SUBCUTANEOUS	Dec. 22, 2026	NEW CHEMICAL ENTITY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Proprotein convertase subtilisin/kexin type 9	Enzyme	Q8NBP7	PCSK9_HUMAN	ANTISENSE INHIBITOR	IC50	11.54		DRUG LABEL	DRUG LABEL

External reference:

ID	Source
CHEBI:176399	CHEBI
CHEMBL3990033	ChEMBL_ID
C585830	MESH_SUPPLEMENTAL_RECORD_UI
DB14901	DRUGBANK_ID
018725	NDDF
4041078	VANDF
D11931	KEGG_DRUG
C4307388	UMLSCUI
CHEMBL5095052	ChEMBL_ID
10268	INN_ID
39492511000001108	SNOMEDCT_US
126480325	PUBCHEM_CID
2588243	RXNORM
345011	MMSL
d09728	MMSL
UOW2C71PG5	UNII

Pharmaceutical products:

None